XE991二塩酸塩 化学特性,用途語,生産方法
用途
M電流/KCNQチャンネル阻害剤。
特長
1. KCNQ2+3、M電流およびKCNQ1を強力に阻害します。2. 他の電位依存性K+チャンネルに対し40倍以上の選択性を示します。3. in vitroで、ラット海馬切片からの[3H]アセチルコリン放出量を増加させます。4. ラットへの経口投与後、神経伝達物質の放出量を増加させ、認知力を高めます。
説明
The KCNQ potassium channels are neuronal modulators which combine with other KQT or KCNE channels to form heteromultimers. XE 991 is a blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC
50 = 0.75 and 0.71 μM, respectively) as well as KCNQ2+3 heteromultimers (IC
50 = 0.6 μM). It much less effectively blocks eag, erg, and elk channels. The effectiveness of XE 991 against KCNQ channels depends on partners or accessory proteins. Through these actions, XE 991 enhances acetylcholine release from rat brain slices (EC
50 = 490 nM) and shows good
in vivo potency and duration of action, suggesting utility in Alzheimer’s disease therapeutics. While early studies focused on actions in the central nervous system, XE 991 can be used to explore the roles of KCNQ channels in neuronal regulation throughout the body.
使用
XE 991 dihydrochloride is a potent & selective inhibitor of KCNQ voltage-gated K-channels.
XE991二塩酸塩 上流と下流の製品情報
原材料
準備製品